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Flibanserin

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Chemical Structure| 167933-07-5 同义名 : 氟班色林 ;BIMT-17;BIMT-17BS;Flibanserin. Brand name: Addyi.;EBD6396
CAS号 : 167933-07-5
货号 : A101358
分子式 : C20H21F3N4O
纯度 : 98%
分子量 : 390.402
MDL号 : MFCD00918402
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

生物活性
靶点

  • 5-HT2

    5-HT2A, Ki:49 nM

  • 5-HT1

    5-HT1A, Ki:1 nM
描述 Flibanserin, also named as BIMT 17, is a kind of 5-HT2A receptor antagonist and 5-HT1A receptor full agonist. In vitro studies, it was found that flibanserin showed a good affinity for 5-HT1A and 5-HT2A receptors with the pKi of 7.72 and 6.90 respectively in cerebral cortical, while no appreciable affinity for the other 5-HT receptor subtypes. Besides this, flibanserin could also reduce the forskolin-stimulated cAMP accumulation in the cerebral cortex and in the hippocampus, as well as inhibit the 5-HT-induced phosphatidylinositol turnover in the cerebral cortex[3]. In vivo studies, flibanserin could act as a full agonist in the dorsal raphe nucleus (DRN) and the medial prefrontal cortex (mPFC), but as a partial agonist in the CA3 region of the hippocampus in the rat brain, when applied by the local microiontophoretic[4]. In addition, systemic administration of flibanserin could contribute to the change of some monoamine’s level in rat brain, such as neurotransmitters serotonin (5-HT), norepinephrine (NE) and so on[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00360555 Sexual Dysfunctions, Psycholog... 展开 >>ical 收起 << Phase 3 Completed - -
NCT00491829 Sexual Dysfunctions, Psycholog... 展开 >>ical 收起 << Phase 3 Completed - -
NCT00360555 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL
参考文献

[1]Gao Z, Yang D, et al. Efficacy and Safety of Flibanserin in Women with Hypoactive Sexual Desire Disorder: A Systematic Review and Meta-Analysis. J Sex Med. 2015 Nov;12(11):2095-104.

[2]Simon JA, Kingsberg SA, et al. Efficacy and safety of flibanserin in postmenopausal women with hypoactive sexual desire disorder: results of the SNOWDROP trial. Menopause. 2014 Jun;21(6):633-40.

[3]Borsini F, Giraldo E, Monferini E, Antonini G, Parenti M, Bietti G, Donetti A. BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex. Naunyn Schmiedebergs Arch Pharmacol. 1995 Sep;352(3):276-82. doi: 10.1007/BF00168557. PMID: 8584042.

[4]Rueter LE, de Montigny C, Blier P. In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre- and postsynaptic 5-HT1A receptors in the rat brain. Synapse. 1998 Aug;29(4):392-405. doi: 10.1002/(SICI)1098-2396(199808)29:4<392::AID-SYN11>3.0.CO;2-T. PMID: 9661257.

[5]Allers KA, Dremencov E, Ceci A, Flik G, Ferger B, Cremers TI, Ittrich C, Sommer B. Acute and repeated flibanserin administration in female rats modulates monoamines differentially across brain areas: a microdialysis study. J Sex Med. 2010 May;7(5):1757-67. doi: 10.1111/j.1743-6109.2010.01763.x. Epub 2010 Feb 12. PMID: 20163532.